Home Angiogenesis BTK inhibitor Pirtobrutinib (LOXO-305) For research use only.

Pirtobrutinib (LOXO-305)

Synonyms: LY 3527727, RXC-005

Pirtobrutinib (LOXO-305, LY 3527727, RXC-005) is a highly selective, non-covalent, next generation BTK inhibitor with an IC50 of 5.69 nM in WT BTK HEK cells. Pirtobrutinib shows more than 300-fold selective for BTK over 98% of 370 other kinases.

Pirtobrutinib (LOXO-305) Chemical Structure

Pirtobrutinib (LOXO-305) Chemical Structure

CAS No. 2101700-15-4

Purity & Quality Control

Pirtobrutinib (LOXO-305) Related Products

Signaling Pathway

BTK Signaling Pathways

BTK Signaling Pathway

Biological Activity

Description

Pirtobrutinib (LOXO-305, LY 3527727, RXC-005) is a highly selective, non-covalent, next generation BTK inhibitor with an IC50 of 5.69 nM in WT BTK HEK cells. Pirtobrutinib shows more than 300-fold selective for BTK over 98% of 370 other kinases.
Targets
BTK [1]
(in WT BTK HEK cells)
5.69 nM
In vitro
In vitro

Pirtobrutinib (LOXO-305) is a highly selective, non-covalent, next-generation Bruton's tyrosine kinase (BTK) inhibitor, which potently inhibits the cellular activity of BTK C481S, T and R mutations and displays strong equilibrium binding to WT BTK and several BTK C481 substitution mutations.<sup><a class="sref" href="#s_ref">[2]</a></sup>
Cell Research Cell lines WT BTK HEK293T cells
Concentrations --
Incubation Time 2 h
Method

HEK293T cell lines transiently expressing WT BTK and BTK C481 substitution mutations were incubated with LOXO-305, ibrutinib or acalabrutinib for 30 min followed by the addition of orthovanadate. After 2 h, cells were lysed, and phosphorylated Y223 BTK and total BTK levels were detected by immunoblot (BTK WT, C481S, and C481T) or MesoScale (C481R). Bands and MSD signals were quantified, and the IC50 values calculated with GraphPad Prism.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06104683 Withdrawn
Relapsing Multiple Sclerosis|Multiple Sclerosis
Loxo Oncology Inc.|Eli Lilly and Company
 May 1 2024 Phase 2
NCT05990465 Not yet recruiting
Non Hodgkin Lymphoma|Diffuse Large B Cell Lymphoma|Follicular Lymphoma|Marginal Zone Lymphoma|Mantle Cell Lymphoma|Burkitt Lymphoma
Medical College of Wisconsin
 April 2024 Phase 1
NCT06333262 Recruiting
Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma
Inhye Ahn|Loxo Oncology Inc.|Dana-Farber Cancer Institute
 April 22 2024 Phase 2
NCT06258174 Completed
Healthy
Eli Lilly and Company|Loxo Oncology Inc.
 September 28 2021 Phase 1
NCT05023980 Active not recruiting
Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma
Loxo Oncology Inc.|Eli Lilly and Company
 September 23 2021 Phase 3

Chemical Information & Solubility

Molecular Weight 479.43 Formula

C22H21F4N5O3
CAS No. 2101700-15-4 SDF --
Smiles COC1=CC=C(F)C=C1C(=O)NCC2=CC=C(C=C2)C3=N[N](C(C)C(F)(F)F)C(=C3C(N)=O)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 96 mg/mL ( (200.23 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 48 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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